R306465

Research use only, not for human use.

R306465 (JNJ-16241199) is an orally active and selective class I histone deacetylase (HDAC 1) inhibitor with an IC50 of 3.3 nM.

JNJ-16241199 is an orally active, selective hydroxamate-based histone deacetylase (HDAC)inhibitor, with the IC50 of 3.3 nM and 23 nM for HDAC1 and HDAC8, respectively. JNJ-16241199 induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells. JNJ-16241199 induces cell apoptosis and shows anticancer activity in a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study.

Cell Cycle Analysis Cell Line:Human A2780 ovarian carcinoma cells Concentration:0, 0.1, 0.3, 1 μM Incubation Time:24 h or 48 h Result:Decreased in S phase at 300 nM, with a parallel increase in G1 phase, but increased in the sub-G1 fraction of cells at the 1 μM after 24 h. Increased in sub-G1 phase at all active concentrations starting from 100 nM after 48 h.

Animal Model:Human A2780, H460 and HCT116 orthotopic xenograft tumor modelsDosage:10-40 mpk/day for 28 days Administration:Oral gavage (p.o.)Result:Induced H3 acetylation and p21waf1, cip1 promoter activity in A2780 ovarian tumour tissue. Decreased tumour volume in three orthotopic xenograft tumor models. Reached maximal decrease in final tumour volume to 76–87% in human A2780 orthotopic xenograft tumor models.

——

Cell Cycle/DNA Damage

HDAC

HDAC | Apoptosis

——

——

604769-01-9

413.45

C19H19N5O4S

>98% (HPLC)

——

O=C(NO)C1=CN=C(N=C1)N2CCN(CC2)S(=O)(=O)C=3C=CC=4C=CC=CC4C3

——

(-20℃)

With Ice Pack

≥ 2 years